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    Gemcitabine HCl
    Gemcitabine HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1423
    CAS #: 122111-03-9Purity ≥98%

    Description: Gemcitabine HCl (formerly also known as LY-188011, NSC-613327; dFdC; dFdCyd; trade name: Gemzar), the hydrochloride salt of gemcitabine which is an antimetabolite anticancer drug, is a potent DNA synthesis inhibitor approved for cancer treatment. It inhibits DNA synthesis with IC50s of 50 nM, 40 nM, 18 nM and 12 nM in PANC1, MIAPaCa2, BxPC3 and Capan2 cells, respectively. Gemcitabine is converted intracellularly to the active metabolites difluorodeoxycytidine di- and triphosphate (dFdCDP, dFdCTP). dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis.

    References: Oncology. 2002;62(4):354-62; J Gastrointest Surg. 2012 Jul;16(7):1333-40.

    Related CAS#: 95058-81-4 (free base); 210829-30-4 [Gemcitabine elaidate, also known as CO-101 and CP-4126, is a lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC)]; 116371-67-6 (Gemcitabine monophosphate free acid); 1638288-31-9 (Gemcitabine monophosphate disodium salt); 840506-29-8 [Acelarin (NUC-1031) is a ProTide transformation and enhancement of the widely-used nucleoside analogue, gemcitabine]; 892128-60-8 (LY2334737, an orally bioavailable prodrug of gemcitabine)

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    Molecular Weight (MW)299.66
    CAS No.122111-03-9; 95058-81-4 (free base);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: <1 mg/mL
    Water: 19 mg/mL (63.4 mM)
    Ethanol:<1 mg/mL (slightly soluble or insoluble)
    Solubility (In vivo)Saline: 20 mg/mL

    Abbreviations: dFdC; dFdCyd; LY188011; LY-188011; LY 188011; gemcitabine; Gemzar.

    Chemical Name: 4-amino-1-((2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one hydrochloride

    SMILES Code: O=C1N=C(N)C=CN1[[email protected]@H]2O[[email protected]](CO)[[email protected]@H](O)C2(F)F.[H]Cl

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    In Vitro

    In vitro activity: Gemcitabine induced NF-κB activity in BxPC-3, PANC-1, and MIA PaCa-2 cells and decreased the level of the NF-κB inhibitor IκBα in BxPC-3 and PANC-1 cells. Treatment of BxPC-3 cells with low dose Gemcitabine for 48 hours results in a dose-dependent increase in NF-κB binding. In contrast, NF-κB DNA binding is decreased in BxPC-3 cells treated with the higher Gemcitabine doses for 48 h; however, 24-h treatment with these higher doses increases NF-κB binding in BxPC-3 cells.

    Cell Assay: BxPC-3, MIA PaCa-2, and PANC-1 cells are seeded in a 96-well plate. After 24 hours, cells are treated with vehicle, DMAPT and/or Gemcitabine for an additional 24 hours or 48 hours. Apoptosis is quantified using the Cell Death Detection ELISA to detect the amount of cytoplasmic histone-associated DNA fragments and expressed relative to vehicle-treated cells.

    In VivoIntratumoral NF-κB activity is significantly elevated (1.3- to 1.8-fold) in the Gemcitabine-treated mice compared to the PBS-treated mice, suggesting that Gemcitabine also induces NF-κB activation.
    Animal modelAthymic nude mice with MIA PaCa-2 cells
    Formulation & DosageDissolved in PBS; 50 or 100 mg/kg; i.p. injection
    ReferencesOncology. 2002;62(4):354-62; J Gastrointest Surg. 2012 Jul;16(7):1333-40.

    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Gemcitabine HCl


    Gemcitabine HCl


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